Registration now open for Medicinal Chemistry Residential School 2014
With a 40 year history in the UK, the Royal Society of Chemistry Medicinal Chemistry Residential School has trained some of the world’s leading medicinal chemists working in the pharmaceutical industry. Now, for the first time, this highly successful course will be coming to Asia – from 20-23 November, Shangai, China.
Do you want to develop your medicinal chemistry skills?
This 3-day course strengthens excellence in medicinal chemistry by highlighting best practice and facilitating understanding of the factors governing modern drug discovery.
What you will learn
The course covers all aspects of drug discovery. A full list of themes is on our website. These topics will be explored through a varied programme of lectures, case histories, and hands-on tutorial sessions.
Who you will learn from
This is a truly unique opportunity for discussions and networking with peers and internationally recognised leaders in the field. See our list of prestigious speakers.
Registration is now open. There are limited spaces available on the course so make sure you register as soon as possible.
Check out the following HOT articles, these have been made free to access for a limited time:
Recognition of diazirine-modified O-GlcNAc by human O-GlcNAcase
Andrea C. Rodriguez and Jennifer J. Kohler
Med. Chem. Commun., 2014,5, 1227-1234
Free to access until 21st August 2014
Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition
Phillip P. Sharp, Jean-Marc Garnier, David C. S. Huang and Christopher J. Burns
Med. Chem. Commun., 2014, Advance Article
Free to access until 21st August 2014
Beyond substrate analogues: new inhibitor chemotypes for glycosyltransferases
Lauren Tedaldi and Gerd K. Wagner
Med. Chem. Commun., 2014,5, 1106-1125
Free to access until 21st August 2014
RSC Organic Division Poster Symposium 2014, headline sponsored by F. Hoffmann-La Roche, Ltd.
The poster symposium, for final year organic chemistry PhD students, will take place at The Royal Society of Chemistry, Burlington House, London on Monday 01 December 2014.
The symposium offers final year PhD students a chance to showcase their research to their peers, leading academics and industrial chemists, and is open to all branches of organic chemistry. The symposium has a tradition of being the most competitive and highly regarded organic chemistry symposium for PhD students in the UK and ROI and we would like to thank F. Hoffmann-La Roche, Ltd. for their generous support of the event.
There will be a first prize of £500, two runner-up prizes of £250, and a “selected by Industry Prize”. Industrial delegates will make this selection by considering the research’s potential for application in an industrial context; the winner will also receive a prize of £500.
Closing date for submissions is Wednesday 01 October 2014.
For more information and to submit your abstract go to http://rsc.li/organic-poster
Every two years the European Federation for Medicinal Chemistry (EFMC), a partner society of MedChemComm, honour three awards at the International Symposium on Medicinal Chemistry (EFMC-ISMC). Congratulations to the following winners of the EFMC Awards 2014!
Nauta Award for Pharmacochemistry
Professor Paul Leeson
UCB-Ehrlich Award for Excellence in Medicinal Chemistry
Professor Craig Crews
Yale University, Department of Chemistry, New Haven, USA
Prous Institute-Overton and Meyer Award for New Technologies in Drug Discovery
Professor György Ferenczy and Professor György Keseru
Research Centre for Natural Sciences, Hungarian Academy of Sciences, Budapest, Hungary
These awards acknowledge outstanding achievements in the field of Medicinal Chemistry.
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A very successful Kinase 2014 was held on 19-20 May 2014 with some great talks and interesting perspectives being presented on the future of kinase inhibitor research.
Eight VIP Chinese Pharmaceutical Association (CPA) delegates attended the Kinase 2014 held at the Babraham Research Institute in Cambridge. Three of the CPA delegates presented their research at the meeting which also included a lecture from Nathanael S Gray (Harvard), recent guest editor for Med Chem Comm themed issue “Chemical Biology for Target Identification and Validation”.
Jeff Kropf (Gilead Sciences) won the MedChemComm prize for his research on the discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase (Syk).
Charlotte Griffiths-Jones (Astex Pharmaceuticals) won the CBID prize for her poster on fragment based drug discovery of selective inhibitors of fibroblast growth facter receptor (FGFR).
Nominations for the MedChemComm Emerging Investigator Lectureship are now open. This annual Lectureship recognises an emerging scientist who has made a significant contribution to medicinal chemistry or a related field in the early part of their independent career.
To make a nomination, please contact the MedChemComm Editorial Office with the name and affiliation of the person you are nominating. Nominees must have completed their PhD on or after the 31st December 2004.
Closing date for Nominations is the 30th June 2014
The decision to award the Lectureship will be made by a panel of MedChemComm Editorial Board members. The recipient will receive a contribution towards speaking at a conference. Previous Lectureship winners are Professor Patrick Gunning (University of Toronto, Canada) and Professor Christian Heinis (École Polytechnique Fédérale de Lausanne, Switzerland).
Decreased biosynthesis of hydrogen sulfide is found in a range of disease states. In cell based assays, hydrogen sulfide can prevent oxidant-induced cell damage. Together, these findings suggest that strategies to increase hydrogen sulfide bioavailability may have potential in the treatment of disease states such as hypertension and diabetes.
A recent article published in MedChemComm reports the synthesis of a hydrogen sulfide donor molecule coupled to a triphenylphosphonium cation (AP39).
The effects of this molecule on oxidative stress were compared against a compound with known vasodilatory activity in a cellular model. Lipophilic cation, such as the triphenylphosphonium cation, can accumulate within mitochondria (the main source of detrimental oxidant production within cells). The cytoprotective potency of the synthesised compound was greater than that of the comparator, suggesting that compounds capable of delivering hydrogen sulfide to mitochondria may have therapeutic potential.
The synthesis and functional evaluation of a mitochondria-targeted hydrogen sulfide donor, (10-oxo-10-(4-(3-thioxo-3H-1,2-dithiol-5-yl)phenoxy)decyl)triphenylphosphonium bromide (AP39)
Sophie Le Trionnaire, Alexis Perry, Bartosz Szczesny, Csaba Szabo, Paul G. Winyard, Jacqueline L. Whatmore, Mark E. Wood and Matthew Whiteman
Med. Chem. Commun., 2014, DOI: 10.1039/C3MD00323J, Concise Article
Please take a look at the following articles which were the Top Ten most accessed during January, February and March!
Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011,2, 1135-1161
Amidines bearing benzofuroxan or benzimidazole 1,3-dioxide core scaffolds as Trypanosoma cruzi-inhibitors: structural basis for their interactions with cruzipain
Alicia Merlino, Diego Benitez, Nuria E. Campillo, Juan A. Páez, Luzineide W. Tinoco, Mercedes González and Hugo Cerecetto
Med. Chem. Commun., 2012,3, 90-101
Discovery of BET bromodomain inhibitors and their role in target validation
S. Müller and S. Knapp
Med. Chem. Commun., 2014,5, 288-296
Metabolism-guided drug design
Antonia F. Stepan, Vincent Mascitti, Kevin Beaumont and Amit S. Kalgutkar
Med. Chem. Commun., 2013,4, 631-652
3-Hydroxylation of the polycyclic tetramate macrolactam in the biosynthesis of antifungal HSAF from Lysobacter enzymogenes C3
Yaoyao Li, Justin Huffman, Yu Li, Liangcheng Du and Yuemao Shen
Med. Chem. Commun., 2012,3, 982-986
Affinity-based target identification for bioactive small molecules
Makoto Kawatani and Hiroyuki Osada
Med. Chem. Commun., 2014,5, 277-287
Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments
Charlotte E. Allen, Amanda J. Welford, Thomas P. Matthews, John J. Caldwell and Ian Collins
Med. Chem. Commun., 2014,5, 180-185
Ambient mass spectrometry technologies for the detection of falsified drugs
María J. Culzoni, Prabha Dwivedi, Michael D. Green, Paul N. Newton and Facundo M. Fernández
Med. Chem. Commun., 2014,5, 9-19
Microwave-assisted synthesis of N-heterocycles in medicinal chemistry
Davide Garella, Emily Borretto, Antonella Di Stilo, Katia Martina, Giancarlo Cravotto and Pedro Cintas
Med. Chem. Commun., 2013,4, 1323-1343
Target validation using in-cell small molecule clickable imaging probes
Brahma Ghosh and Lyn H. Jones
Med. Chem. Commun., 2014,5, 247-254
If you have any thoughts or comments on any of these articles, please leave these in the comment box below!
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